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Description: S1RA HCl (also known as E-52862 HCl) is a potent and selective sigma-1 receptor(sigma1R, Ki=17 nM) antagonist, showed good selectivity against sigma2R (Ki > 1000 nM). E-52862 showed high activity in the mouse capsaicin model of neurogenic pain, emerged as the most interesting candidate. In addition, compound 28 exerted dose-dependent antinociceptive effects in several neuropathic pain models. This, together with its good physicochemical, safety, and ADME properties, led compound 28 to be selected as clinical candidate.
References: Br J Pharmacol. 2012 Aug; 166(8):2289-306; J Med Chem. 2012 Oct 11; 55(19):8211-24.
Related CAS#: 878141-96-9 (free base); 1265917-14-3 (HCl)
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